benzofurans and fluorexon

Cisplatin resistance in ovarian cancer remains a complex problem as tumors frequently develop resistance against drugs, a mechanism sometimes mediated by ATP-Binding Cassette transporters. Our goal was to find compounds restricting their inhibition capacity to the cisplatin efflux mediated by ABCC2 pump, among previously identified inhibitors, derived from the 2- indolylmethylenebenzofuranones. Methodology & results: An original method setup allows direct quantitation of platinum by employing cyTOF mass cytometry. Among tested derivatives, some led to a full platinum accumulation and efficiently resensitized cisplatin-resistant A2780 cells to cisplatin while preserving most of the calcein efflux activity.. CyTOF is therefore a powerful and promising method to quantify cisplatin accumulation that may be used in the clinical setting to improve and personalize cancer treatment.

Topics: Antineoplastic Agents; Benzofurans; Cell Line, Tumor; Cell Survival; Cisplatin; Drug Resistance, Neoplasm; Female; Fluoresceins; Humans; Multidrug Resistance-Associated Protein 2; Multidrug Resistance-Associated Proteins; Ovarian Neoplasms